Abstract
The increasing drug resistance of malaria parasites challenges the treatment of this life-threatening disease. Consequently, the development of innovative and effective antimalarial drugs is inevitable. O-tigloylcyclovirobuxeine-B, a nor-cycloartane alkaloid from Buxus sempervirens L., has shown promising and selective in vitro activity in previous studies against Plasmodium falciparum (Pf), causative agent of Malaria tropica. For further investigations, it is indispensable to develop an advanced and efficient isolation procedure of this valuable natural product. Accordingly, we used liquid–liquid chromatography including centrifugal partition chromatography (CPC) to obtain the pure alkaloid on a semi-preparative scale. Identification and characterization of the target compound was accomplished by UHPLC/+ESI-QqTOF-MS/MS, 1H NMR and 13C NMR. In conclusion, this work provides a new and efficient method to obtain O-tigloylcyclovirobuxeine-B, a valuable natural product, as a promising antiplasmodial lead structure for the development of innovative and safe medicinal agents.
Highlights
Buxus sempervirens L. (European Box; Buxaceae) is an indeciduous shrub, which represents a rich source for nor-triterpene alkaloids of the nor-cycloartane type
1.5of kgtarget of dried plant material, advantages in using thispartition all-liquid separation scheme are diverse, including a high recovery onlyThe three steps of liquid–liquid (one acid/base partitioning step and two steps of centrifugal of injectedchromatography sample, a low solvent, tailing of eluted partition (CPC))consumption were required in order obtain
Our findings demonstrate that centrifugal partition chromatography (CPC) is an advantageous chromatographic technique for natural compound isolation in case of amino nor-cycloartane-type alkaloids from Buxus
Summary
Buxus sempervirens L. (European Box; Buxaceae) is an indeciduous shrub, which represents a rich source for nor-triterpene alkaloids of the nor-cycloartane type. (European Box; Buxaceae) is an indeciduous shrub, which represents a rich source for nor-triterpene alkaloids of the nor-cycloartane type. Decoctions of the leaves are well known in folk medicine for a variety of indications, including malaria [1,2]. Malaria is a poverty-related infectious disease caused by protozoans of the genus Plasmodium and transmitted by infected female Anopheles mosquitoes. Worldwide there were 228 million estimated malaria cases in. The development of new effective agents against this life-threatening disease is imperative because of increasing drug resistance. Extracts of the leaves from B. sempervirens L. have shown selective in vitro activity against
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